633698-29-0Relevant articles and documents
From bradykinin B2 receptor antagonists to orally active and selective bradykinin B1 receptor antagonists
Barth, Martine,Bondoux, Michel,Luccarini, Jean-Michel,Peyrou, Vincent,Dodey, Pierre,Pruneau, Didier,Massardier, Christine,Paquet, Jean-Luc
, p. 2574 - 2584 (2012/05/20)
The bradykinin (BK) B1 receptor is an attractive target for the treatment of chronic pain and inflammation. Starting from a dual B1 and B2 antagonist, novel antagonists were designed that display low-nanomolar affinity for human B1 receptor and selectivity over B2. Initially, potent imidazoline derivatives were studied, but these compounds suffered from low bioavailability. This issue could be overcome by the use of less basic amino derivatives leading to orally active compounds.
Novel arylsulphonamide derivatives and use thereof as therapeutic agents
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Page/Page column 18, (2008/06/13)
The present invention relates to novel arylsulphonamide compounds, defined by formula I and the description, as well as their method of preparation and their therapeutic use.